Referencia número: HY-117410

Vipivotide tetraxetan

(Synonyms: PSMA-617)

17 Cited Publications

Revisión del cliente

Based on 17 publication(s) in Google Scholar

Vipivotide tetraxetan (PSMA-617) is a high potent prostate-specific membrane antigen (PSMA) inhibitor, with a K_i of 0.37 nM. Vipivotide tetraxetan (PSMA-617) is designed consisting of three components: the pharmacophore Glutamate-urea-Lysine, the chelator DOTA able to complex both 68Ga or 177Lu, and a linker connecting these two entities. Glutamate-urea-Lysine is the selective pharmacophore to bind to prostate specific membrane antigen.

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Pureza: 99.46%
No. CAS: 1702967-37-0
Fòrmula: C₄₉H₇₁N₉O₁₆
Peso molecular:1042.14

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Vipivotide tetraxetan Chemical Structure

No. CAS: 1702967-37-0

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (17)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target

Traditional Cytotoxic Agents

Ver todos los productos específicos de isoformas Drug-Linker Conjugates for ADC :

In Vitro

Vipivotide tetraxetan (PSMA-617) demonstrates high radiolytic stability for at least 72 h. A high inhibition potency (equilibrium dissociation constant K_i=2.34±2.94 nM on LNCaP; K_i=0.37±0.21 nM enzymatically determined) and highly efficient internalization into LNCaP cells are demonstrated^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Organ distribution with 68Ga-labeled Vipivotide tetraxetan (PSMA-617) after 1 h (n=3) reveals a high specific uptake in LNCaP tumors and in the kidneys. The high uptake in the kidneys is nearly completely blocked by coinjection of 2 mg of 2-PMPA per kilogram. Other organs such as the liver, lung, and spleen show rather low uptake and no blocking effect, with the exception of the spleen. Tumor-to-background ratios are 7.8 (tumor to blood) and 17.1 (tumor to muscle) at 1 h after injection. As compared with the 68Ga-labeled version, the organ distribution with 177Lu-labeled Vipivotide tetraxetan (PSMA-617) (n=3) show a similar uptake in the LNCaP tumors and in the kidneys. The liver uptake is found to be statistically different. Tumor-to-background ratios determined 1 h after injection show slightly higher values (tumor to blood, 22.1; tumor to muscle, 25.6) than previous organ distribution with 68Ga-labeled Vipivotide tetraxetan (PSMA-617)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 1702967-37-0
Appearance Solid
Peso molecular 1042.14
Fòrmula C₄₉H₇₁N₉O₁₆
Color White to off-white
SMILES

O=C(O)[C@H](CCCCNC([C@H](CC1=CC=C2C=CC=CC2=C1)NC([C@H]3CC[C@H](CNC(CN4CCN(CC(O)=O)CCN(CC(O)=O)CCN(CC(O)=O)CC4)=O)CC3)=O)=O)NC(N[C@H](C(O)=O)CCC(O)=O)=O
Synonyms

PSMA-617
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (17)

All In Vivo Efficacy Study

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Biosens Bioelectron

Low cost, high temporal resolution optical fiber-based γ-photon sensor for real-time pre-clinical evaluation of cancer-targeting radiopharmaceuticals. [Abstract]

2024 Mar 1:247:115956. PMID: 38145595

Vipivotide tetraxetan purchased from MedChemExpress. Usage Cited in: Biosens Bioelectron. 2024 Mar 1:247:115956. [Abstract]

SPECT scans show progression of 177Lu-Vipivotide tetraxetan (PSMA-617) (i.v.) activity accumulation in PC3-PIP and PC3-flu tumors at five time points taken at the end of every custom γ-probe recording.
J Nucl Med

Preclinical Evaluation of 177Lu-rhPSMA-10.1, a Radiopharmaceutical for Prostate Cancer: Biodistribution and Therapeutic Efficacy. [Abstract]

2025 Apr 1;66(4):599-604. PMID: 40049746

Vipivotide tetraxetan purchased from MedChemExpress. Usage Cited in: J Nucl Med. 2025 Apr 1;66(4):599-604. [Abstract]

177Lu-Vipivotide tetraxetan (PSMA-617) (30 MBq) significantly suppressed tumor growth from day 18 to day 35 and was well tolerated in the LNCaP xenograft-bearing mice, and no significant weight loss was noted.
Eur J Nucl Med Mol Imaging

Preliminary evaluation of a novel PSMA-targeting radiopharmaceutical [68Ga]Ga/[177Lu]Lu-NYM032 for theranostic use in prostate cancer. [Abstract]

2025 Apr;52(5):1671-1684. PMID: 39745526

Vipivotide tetraxetan purchased from MedChemExpress. Usage Cited in: Eur J Nucl Med Mol Imaging. 2025 Apr;52(5):1671-1684. [Abstract]

Representative torso MIP, CT, and PET/CT imaging with [68Ga]Ga-NYM032 and [68Ga]Ga-Vipivotide tetraxetan (PSMA617) (111 MBq/patient) were performed on the same PCa patients. [68Ga]Ga-Vipivotide tetraxetan (PSMA617) showed good diagnostic efficiency for primary, recurrent, and metastatic PCa lesions.
Eur J Nucl Med Mol Imaging

[177Lu]Lu-PSMA-617 theranostic probe for hepatocellular carcinoma imaging and therapy. [Abstract]

2023 Jul;50(8):2342-2352. PMID: 36877233

Vipivotide tetraxetan purchased from MedChemExpress. Usage Cited in: Eur J Nucl Med Mol Imaging. 2023 Jul;50(8):2342-2352. [Abstract]

Representative SPECT images and biodistribution of HepG2 tumor-bearing mice injected with [177Lu]Lu-Vipivotide tetraxetan (PSMA-617) (37 MBq). Tumor uptake of [177Lu]Lu- Vipivotide tetraxetan (PSMA-617) decreased over time indicating rapid blood clearance and short tumor retention time.

Vipivotide tetraxetan purchased from MedChemExpress. Usage Cited in: Eur J Nucl Med Mol Imaging. 2023 Jul;50(8):2342-2352. [Abstract]

Efficacy of radioligand therapy of HepG2 tumor-bearing mice models injected with a single dose of [177Lu]Lu-Vipivotide tetraxetan (PSMA-617) (37 MBq) and [177Lu]Lu-EB-Vipivotide tetraxetan (PSMA-617). Treatment groups exhibited significantly reduced tumor volume and weight compared with the saline group.
Int J Radiat Oncol Biol Phys

SENTRI: Single-particle Energy Transducer for Radionuclide Injections for Personalized Targeted Radionuclide Cancer Therapy. [Abstract]

2024 Apr 1;118(5):1575-1584. PMID: 38122990
Pharmaceutics

Hematological Toxicity in Mice after High Activity Injections of 177Lu-PSMA-617. [Abstract]

2022 Mar 28;14(4):731. PMID: 35456565
Mol Ther Nucleic Acids

Highly efficient nucleic acid encapsulation method for targeted gene therapy using antibody conjugation system. [Abstract]

2024 Sep 5;35(4):102322. PMID: 39363882
Pharmaceuticals (Basel)

Characterization of Non-Specific Uptake and Retention Mechanisms of [177Lu]Lu-PSMA-617 in the Salivary Glands. [Abstract]

2023 May 3;16(5):692. PMID: 37242475
Pharmaceuticals (Basel)

Albumin-Mediated Size Exclusion Chromatography: The Apparent Molecular Weight of PSMA Radioligands as Novel Parameter to Estimate Their Blood Clearance Kinetics. [Abstract]

2022 Sep 19;15(9):1161. PMID: 36145382
Biomolecules

177Lu-PSMA-617 Therapy in Mice, with or without the Antioxidant α1-Microglobulin (A1M), Including Kidney Damage Assessment Using 99mTc-MAG3 Imaging. [Abstract]

2021 Feb 10;11(2):263. PMID: 33579037
Sci Rep

2024 May 11.
Mol Pharm

Evaluation of a Radio-IMmunoStimulant (RIMS) in a Syngeneic Model of Murine Prostate Cancer and ImmunoPET Analysis of T-cell Distribution. [Abstract]

2022 Sep 5;19(9):3217-3227. PMID: 35895995
Nucl Med Biol

Enhancing the therapeutic index of [211At]YF2 with iodo pseudo carrier: A simple strategy for reducing accumulation in kidneys, salivary and lacrimal glands. [Abstract]

2025 May 11:146-147:109028. PMID: 40393125
Cancer Biother Radiopharm

Intratumoral Distribution of [177Lu]Lu-PSMA-617 Over Time and in Relation to Diagnostic Tracers in Animal Models of Prostate Cancer. [Abstract]

2025 Apr;40(3):219-227. PMID: 39605131
J Labelled Comp Radiopharm

Automated radiolabeling and handling of 177 Lu- and 225 Ac-PSMA-617 using a robotic pipettor. [Abstract]

2024 Mar;67(3):111-115. PMID: 38296817
Seoul National University

2025 Jan.
Res Sq

2025 Feb 19.

Solvente y solubilidad

In Vitro:

DMSO : 100 mg/mL (95.96 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : ≥ 100 mg/mL (95.96 mM)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

0.9596 mL

4.7978 mL

9.5956 mL

5 mM

0.1919 mL

0.9596 mL

1.9191 mL

10 mM

0.0960 mL

0.4798 mL

0.9596 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (2.00 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (2.00 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (2.00 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact

MedChemExpress (MCE) .

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (273 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Benešová M, et al. Preclinical Evaluation of a Tailor-Made DOTA-Conjugated PSMA Inhibitor with Optimized Linker Moiety for Imaging and Endoradiotherapy of Prostate Cancer. J Nucl Med. 2015 Jun;56(6):914-20. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO / H₂O	1 mM	0.9596 mL	4.7978 mL	9.5956 mL	23.9891 mL
	5 mM	0.1919 mL	0.9596 mL	1.9191 mL	4.7978 mL
	10 mM	0.0960 mL	0.4798 mL	0.9596 mL	2.3989 mL
	15 mM	0.0640 mL	0.3199 mL	0.6397 mL	1.5993 mL
	20 mM	0.0480 mL	0.2399 mL	0.4798 mL	1.1995 mL
	25 mM	0.0384 mL	0.1919 mL	0.3838 mL	0.9596 mL
	30 mM	0.0320 mL	0.1599 mL	0.3199 mL	0.7996 mL
	40 mM	0.0240 mL	0.1199 mL	0.2399 mL	0.5997 mL
	50 mM	0.0192 mL	0.0960 mL	0.1919 mL	0.4798 mL
	60 mM	0.0160 mL	0.0800 mL	0.1599 mL	0.3998 mL
	80 mM	0.0120 mL	0.0600 mL	0.1199 mL	0.2999 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Keywords

Vipivotide tetraxetan

17 Cited Publications

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Vipivotide tetraxetan

Publications Citing Use of MedChemExpress (MCE) Vipivotide tetraxetan

Ver todos los productos específicos de isoformas Drug-Linker Conjugates for ADC

Actividad biológica

Chemical Information

Publications (17)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Vipivotide tetraxetan Related Classifications

HY-117410 Related Classifications